7-Methoxy-1,3,11,12,14,15,16,17,18,19,20,21-dodecahydroyohimban-18-ol

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吲哚及其衍生物
• 英文名称: 7-Methoxy-1,3,11,12,14,15,16,17,18,19,20,21-dodecahydroyohimban-18-ol
• 英文别名: 7-methoxy-1,3,11,12,14,15,16,17,18,19,20,21-dodecahydroyohimban-18-ol
• 化学式: C₂₀H₂₆N₂O₂
• 分子量: 326.4
• InChiKey: WXIHPLPCIHRBPL-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.9
• 重原子数：
  24
• 可旋转键数：
  1
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.6
• 拓扑面积：
  48.5
• 氢给体数：
  2
• 氢受体数：
  3

文献信息

• ANTIPSYCHOTIC AGENTS AND STANDARDIZED ANTIPSYCHOTIC FRACTIONS FROM RAUWOLFIA TETRAPHYLLA AND PROCESS OF THEIR ISOLATION
  申请人：Srivastava Santosh Kumar

  公开号：US20120184576A1

  公开（公告）日：2012-07-19

  The present invention relates to bioactive extracts its fractions and isolation of compound from Rauwolfia tetraphylla . The extracts and fractions are useful for the treatment of psychosis based on in-vivo validation on animal model and proportional binding affinities for dopaminergic-D 2 , Cholinergic (muscarinic) and Serotonergic (5HT 2A ) receptors for antipsychotic activity. The present invention relates to novel antipsychotic activity in the leaf alkaloids of Formula 1 and 2 named tetrahydroalstonine, 10-methoxytetrahydroalstonine, isoreserpiline, 10-derαethoxyreserpiline, 11-demethoxyreserpiline, reserpiline and α-yohimbine. The present invention also relates to processes for obtaining antipsychotic extracts as well as for the isolation of alkabids of formula 1 and 2 from the leaves of Rauwolfia tetraphylla . The present invention particularly relates to significant antipsychotic activity in the MeOH extract, ethylacetate and chloroform fractions of R. tetraphylla and in the isolated compounds α-yohimbine, reserpiline and in a mixture 10-demethoxyreserpiline and 11-demethoxyreserpiline in 1:1.5 ratios for treating psychosis without any extra pyramidal symptoms (EPS). 1. R 1 =R 2 =OMe R 3 =β-H (Isoreserpiline) 2. R 1 =R 2 =OMe R 3 =β-H (Reserpiline) ″3. R 1 =OMe R 2 =HR 3 =β-H ( 11 -Demethoxy reserpiline) ″ 4. R 1 =H R 2 =OMe R 3 =β-H (10-Demethoxy reserpiline) ″5. R 1 =R 2 =H R 3 =α-H (Tetrahydroalstonine) * 7 . R 1 =OMe R 2 =H R 3 =α-H (10-Methoxytetrahudroalstonine).
• US9018226B2
  申请人：——

  公开号：US9018226B2

  公开（公告）日：2015-04-28